We report the synthesis, radiosynthesis, and characterization of a radioligand for poly(ADP-ribose) polymerase (PARP). PARP is of central importance in cell homeostasis, neuroplasticity, and neurodegeneration in the brain. A radiolabeled PARP inhibitor was developed and used for autoradiographic quantification of PARP protein concentration in wild-type and transgenic rodent brains ex vivo in high resolution. The binding of [³H]rucaparib was found to be confined to PARP-expressing domains, for example, cerebellar cortex or hippocampal regions in both models. Saturation binding experiments confirmed selective and reversible binding to a single site (K_d = 1.1 ± 0.2 nM).

中文翻译：

---

聚（ADP-核糖）聚合酶在神经变性：ARC SWE tg小鼠中的放射合成和放射性配体结合。

我们报告了合成，放射合成和表征的poly（ADP-核糖）聚合酶（PARP）的放射性配体。PARP在大脑的细胞稳态，神经可塑性和神经退行性变中至关重要。放射性标记的PARP抑制剂被开发并用于在野生型和转基因啮齿动物的脑中PARP蛋白浓度的放射自显影定量体外以高的分辨率。发现[ ³ H] rucaparib的结合仅限于两种模型中的PARP表达域，例如小脑皮质或海马区。饱和结合实验证实了对单个位点的选择性和可逆结合（K _d = 1.1±0.2 nM）。